Lemos, Agostinho; Gomes, Ana Sara; Loureiro, Joana B.; Brandao, Pedro; Palmeira, Andreia; Pinto, Madalena M. M.; Saraiva, Lucilia; Sousa, Maria Emilia published the artcile< Synthesis, biological evaluation, and in silico studies of novel aminated xanthones as potential p53-activating agents>, Safety of 1,2,3,4-Tetrahydroisoquinolin-5-amine, the main research area is aminated xanthone preparation antitumor human docking p53 activator; dimethoxy oxo xanthene carbaldehyde preparation; MDM2-p53 interaction; antitumor activity; computational docking; xanthones; yeast-based assays.
In this work, a series of eleven aminated xanthones possessing a 3,4-dioxygenated pattern of substitution e.g., I was efficiently constructed in moderate to good yields. From this group of compounds, xanthone I was identified for the first time as a putative p53-activating agent, using a yeast-based screening assay. Xanthone I was revealed to inhibit the growth of human HCT116 p53+/+ colon cancer cells, being that this effect was associated with cell cycle arrest through activation of the p53 pathway. Nevertheless, further studies were required to confirm the mechanism of action of compound I, which may lead to the identification of a novel xanthone derivative with promising antitumor activity. These results demonstrated the potential usefulness of coupling amine-containing structural motifs of known MDM2-p53 disruptors into the 3,4-dioxygenated xanthone scaffold as a starting point for the design of novel and improved p53-activating agents with antitumor activity and drug like properties.
Molecules published new progress about Amines Role: PAC (Pharmacological Activity), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 115955-90-3 belongs to class tetrahydroisoquinoline, and the molecular formula is C9H12N2, Safety of 1,2,3,4-Tetrahydroisoquinolin-5-amine.
Referemce:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem